Salification is one of the powerful and widely employed approaches to improve the biopharmaceutical properties of drugs. The FDA’s eighty-year trajectory of new drug approvals depicts around one-third of the drugs clinically used as their pharmaceutical salts. Among various cationic and anionic counterions used in FDA-approved pharmaceutical salts, the carboxylic acids have significantly contributed. A total of 94 pharmaceutical salts discovered during 1943–2020 comprises carboxylic acids as counterions with a major contribution of acetate, maleate, tartrate, fumarate, and succinate. Hydrocodone tartrate is the first FDA-approved carboxylate salt approved in 1943. Overall, the analysis shows that fifteen carboxylic acid counterions are present in FDA-approved pharmaceutical salts with a major share of acetate (18 drugs). This review provides an account of FDA-approved carboxylate salts from 1939 to 2020. The decade-wise analysis indicates that 1991–2000 contributed a maximum number of carboxylate salts (24) and least (3) in 1939–1950. The technical advantage of carboxylate salts over free-base or other counterions is also discussed.

盐化是改善药物生物制药特性的有效且广泛使用的方法之一。FDA 八十年的新药批准轨迹描述了临床上用作其药用盐的药物中约有三分之一。在 FDA 批准的药用盐中使用的各种阳离子和阴离子抗衡离子中，羧酸有显着贡献。1943 年至 2020 年期间发现的总共 94 种药用盐包含作为抗衡离子的羧酸，其中乙酸盐、马来酸盐、酒石酸盐、富马酸盐和琥珀酸盐的主要贡献是。酒石酸氢可酮是 FDA 批准的第一个羧酸盐，于 1943 年获得批准。总体而言，分析表明，在 FDA 批准的药用盐中存在 15 种羧酸抗衡离子，其中醋酸盐占主要份额（18 种药物）。这篇综述提供了 1939 年至 2020 年 FDA 批准的羧酸盐的账户。十年分析表明，1991 年至 2000 年贡献的羧酸盐数量最多（24 种），而 1939 年至 1950 年贡献最少（3 种）。还讨论了羧酸盐相对于游离碱或其他抗衡离子的技术优势。